Enzymatic preparation of an optically active precursor of the CC-1065/duocarmycin pharmacophore

被引:8
作者
Chenevert, R
Courchesne, G
机构
[1] Département de Chimie, Fac. des Sci. et de Genie, Université Laval, Québec
关键词
D O I
10.1246/cl.1997.11
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
Acetylation of 2-[4-(benzyloxy)-2-nitrophenyl]propane-1,3-diol with vinyl acetate in the presence of porcine pancreatic lipase gave the (R)-mono-acetate (ee = 92%). The (S)-mono-acetate was obtained via acetylation of the diol followed by transesterification in ethanol in the presence of the same enzyme. Incorporation of these optically active mono-acetates into the established synthetic routes provided access to both enantiomers of the common pharmacophore of CC-1065/duocarmycin.
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页码:11 / 12
页数:2
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